A Facile One‐Pot Synthesis of New Fused Indole Pyrazole Derivatives and Their Anticancer and Antidiabetic Activities DOI Creative Commons
Senzekile Majola, Myalowenkosi I. Sabela, Robert Moonsamy Gengan

et al.

ChemistrySelect, Journal Year: 2024, Volume and Issue: 9(48)

Published: Dec. 1, 2024

Abstract Indole‐pyrazole hybrids are intriguing due to their potential for synergistic pharmacological effects, unlike molecules with only one pharmacophore. This study presents a one‐pot synthesis of fused indole‐pyrazole derivatives, bis 4a and chromone 4b using an aldehyde, thiosemicarbizide, indole, as anticancer antidiabetic agents. The synthesized compounds were characterized Fourier transform infrared (FTIR), nuclear magnetic resonance (NMR), time‐of‐flight mass spectrometry (TOF‐MS). Initially, mutagenicity test was performed, the showed no significant increase in revertant colonies against Salmonella typhimurium TA 98 100 strains. In MTT assay cytotoxicity two human cancer cell lines, A549 HepG‐2; normal line, HEK 293. Compound high potency IC 50 values 18.70 50.07 µg/mL, respectively, whereas both low inhibition level 293 at µg/mL. vitro α‐amylase α‐glucosidase, compound demonstrated excellent 3.9 µg/mL 12.1 respectively.

Language: Английский

Novel thiazolidin-4-one benzenesulfonamide hybrids as PPARγ agonists: Design, synthesis and in vivo anti-diabetic evaluation DOI
Islam H. Ali, Rasha M. Hassan, Ahmed M. El Kerdawy

et al.

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 269, P. 116279 - 116279

Published: Feb. 29, 2024

Language: Английский

Citations

15
Carvacrol and Thymol Hybrids: Potential Anticancer and Antibacterial Therapeutics DOI Creative Commons
Sijongesonke Peter, Namhla Sotondoshe, Blessing A. Aderibigbe

et al.

Molecules, Journal Year: 2024, Volume and Issue: 29(10), P. 2277 - 2277

Published: May 12, 2024

Cancer is ranked among lethal diseases globally, and the increasing number of cancer cases deaths results from limited access to effective therapeutics. The use plant-based medicine has been gaining interest several researchers. Carvacrol its isomeric compound, thymol, are extracts that possess biological activities, such as antimalarial, anticancer, antifungal, antibacterial. However, their efficacy compromised by poor bioavailability. Thus, medicinal scientists have explored synthesis hybrid compounds containing pharmacophores enhance therapeutic improve Hence, this review a comprehensive report on carvacrol isomer, with potent anticancer antibacterial agents reported between 2020 2024. Furthermore, structural activity relationship (SAR) recommended future strategies further effects will be discussed.

Language: Английский

Citations

9
In silico molecular docking and dynamic simulation of anti-cholinesterase compounds from the extract of Catunaregam spinosa for possible treatment of Alzheimer's disease DOI Creative Commons

Sathish Thandivel,

Poovarasan Rajan,

Tamizharasan Gunasekar

et al.

Heliyon, Journal Year: 2024, Volume and Issue: 10(7), P. e27880 - e27880

Published: March 21, 2024

Alzheimer's disease (AD), is characterized by a progressive loss of cognitive abilities as well behavioral symptoms including disorientation, trouble solving problems, personality and mood changes. Acetylcholinesterase (AChE) promising target for symptomatic improvement in AD due to its consistent early cholinergic deficit. This research has investigated the potential compounds from Catunaregam spinosa AChE inhibitors treatment option AD, aiming enhance neurotransmission alleviate decline. Tacrine, FDA's first approved no longer use hepatotoxicity. Box-Behnken design (BBD) modelling was used optimise ultrasonic extraction alkaloids dried fruits C. spinosa. GC-MS analysis revealed presence ninety phytoconstituents extract. Among them, eighty-nine new are reported this plant fruit time. Out phytoconstituents, eight showed best binding affinity against enzyme, i.e., PDB IDs 1GQR, 1QTI 4PQE targets using iGEMDOCK. The lead hits were tested their drug-like properties atomistic mechanisms silico ADMET prediction, LigPlot analysis, molecular dynamics simulation. results suggest four such 1,4,7,10,13,16-hexaoxacyclooctadecane; butanoic acid, 3-methyl-2-[(phenylmethoxy)imino]-, trime; butane-1,2,3,4-tetraol; D-(+)-ribonic acid.gamma-lactone potent possible AD.

Language: Английский

Citations

6
A Review on the in Vitro and in Vivo Screening of α-Glucosidase Inhibitors DOI Creative Commons

Guangjuan Pan,

Yantong Lu,

Zhiying Wei

et al.

Heliyon, Journal Year: 2024, Volume and Issue: unknown, P. e37467 - e37467

Published: Sept. 1, 2024

Language: Английский

Citations

4
Investigation of the anti-leishmanial potential of triazole-linked carvacrol–coumarin derivatives: a docking, molecular dynamics, MM/GBSA toxicity approach DOI
Caio Henrique Alexandre Roberto, Damião Sampaio de Sousa, Francisco Rogênio da Silva Mendes

et al.

Journal of the Iranian Chemical Society, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 7, 2025

Language: Английский

Citations

0
CO/CO₂ as C1 building blocks: Unveiling new horizons in coumarin synthesis DOI
Zechao Wang, Jiajia Mou, Hao Jia

et al.

Molecular Catalysis, Journal Year: 2025, Volume and Issue: 574, P. 114887 - 114887

Published: Jan. 30, 2025

Language: Английский

Citations

0
In vivo anti-hyperglycemic activity and toxicity evaluation of two bis-coumarin derivative as potential α-glucosidase inhibitors DOI
Maryam Mohammadi‐Khanaposhtani,

Tayebeh Bahrami,

Fatemeh Bandarian

et al.

Journal of Diabetes & Metabolic Disorders, Journal Year: 2025, Volume and Issue: 24(1)

Published: Feb. 13, 2025

Language: Английский

Citations

0
Discovery of antioxidants and α-glycosidase inhibitors from an endophytic fungus Penicillium brefeldianum F4a DOI

Yan Bai,

Feng Guo,

Jiangchun Hu

et al.

Fitoterapia, Journal Year: 2025, Volume and Issue: 182, P. 106479 - 106479

Published: March 11, 2025

Language: Английский

Citations

0
Combating oxi-inflamm-aging: Passerini adducts tethered with 1,2,3-triazoles for enhanced antioxidant defense and 5-LOX inhibition DOI
Mohammed Salah Ayoup,

Magdy Rashwan,

Saied M. Soliman

et al.

RSC Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 1, 2025

Design and synthesis of novel hybrids Passerini adducts tethered with 1,2,3-triazoles as promising dual anti-inflammatory antioxidant agents.

Language: Английский

Citations

0
Coumarin as an Elite Scaffold in Anti-Breast Cancer Drug Development: Design Strategies, Mechanistic Insights, and Structure–Activity Relationships DOI Creative Commons
Atamjit Singh, Karanvir Singh, Kamaljit Kaur

et al.

Biomedicines, Journal Year: 2024, Volume and Issue: 12(6), P. 1192 - 1192

Published: May 27, 2024

Breast cancer is the most common among women. Currently, it poses a significant threat to healthcare system due emerging resistance and toxicity of available drug candidates in clinical practice, thus generating an urgent need for development new potent safer anti-breast candidates. Coumarin (chromone-2-one) elite ring widely distributed natural products possesses broad range pharmacological properties. The unique distribution efficacy coumarins attract product hunters, resulting identification numerous from different sources last three decades, especially those with Inspired by this, synthetic derivatives based on have been developed medicinal chemists all around globe, showing promising efficacy. This review primarily focused coumarin-inspired agents highlighting design strategies, mechanistic insights, their structure–activity relationship. Natural having are also briefly highlighted. will act as guideline researchers designing optimum coumarin-based agents.

Language: Английский

Citations

3